Wednesday, July 10, 2013

Genistein vs Gleevec: natural TKI?

Genistein differs from Gleevec in that genistein is a natural phytoestrogen and targets tyrosine kinase inhibitors (among other things) while Gleevec is a man made small molecule generated to bind specifically to the fusion protein called bcr-abl created by the rearrangement occurring following the break and fusion between chromosomes 9 and 22 specific to CML (GIST also seem to be sensitive to Gleevec). Gleevec works because this fusion protein is present only in tumor cells and it is essential for tumor cell growth. Thus, Gleevec tends to have few side effects and unless the tumor cells develop resistance (which happens in a very small percentage of cases) the drug is effective in killing cells carrying the fusion protein. The presence of a unique protein like bcr-abl is not common in cancers (though others have been identified). So you have the difference between using an nonspecific tki like genistein which is likely to have significant side effects at higher doses as it targets many tkis and has estrogenic activity, and a specific molecule designed to inhibit one specific tyrosine kinase that is known to be involved in tumor cell survival and growth.

   So while the may be some benefits from eating foods containing genistein (besides isoflavones it has anti-oxidant activity) there are doses and side effects to consider - I am also not sure that the amounts present in foods are therapeutically significant. However, before you decide to do any of this and especially if your are thinking of taking supplements, you need to have a discussion with your doctor.


Traganos, Ph.D.
Emeritus Professor of Pathology

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